Early drug discovery and the rise of pharmaceutical chemistry

Drug Test Anal. 2011 Jun;3(6):337-44. doi: 10.1002/dta.301.


Studies in the field of forensic pharmacology and toxicology would not be complete without some knowledge of the history of drug discovery, the various personalities involved, and the events leading to the development and introduction of new therapeutic agents. The first medicinal drugs came from natural sources and existed in the form of herbs, plants, roots, vines and fungi. Until the mid-nineteenth century nature's pharmaceuticals were all that were available to relieve man's pain and suffering. The first synthetic drug, chloral hydrate, was discovered in 1869 and introduced as a sedative-hypnotic; it is still available today in some countries. The first pharmaceutical companies were spin-offs from the textiles and synthetic dye industry and owe much to the rich source of organic chemicals derived from the distillation of coal (coal-tar). The first analgesics and antipyretics, exemplified by phenacetin and acetanilide, were simple chemical derivatives of aniline and p-nitrophenol, both of which were byproducts from coal-tar. An extract from the bark of the white willow tree had been used for centuries to treat various fevers and inflammation. The active principle in white willow, salicin or salicylic acid, had a bitter taste and irritated the gastric mucosa, but a simple chemical modification was much more palatable. This was acetylsalicylic acid, better known as Aspirin®, the first blockbuster drug. At the start of the twentieth century, the first of the barbiturate family of drugs entered the pharmacopoeia and the rest, as they say, is history.

Publication types

  • Historical Article

MeSH terms

  • Alkaloids / analysis
  • Alkaloids / history
  • Alkaloids / isolation & purification
  • Analgesics / chemical synthesis
  • Analgesics / history
  • Analgesics / therapeutic use
  • Antipyretics / chemical synthesis
  • Antipyretics / history
  • Antipyretics / therapeutic use
  • Aspirin / chemical synthesis
  • Aspirin / history
  • Aspirin / therapeutic use
  • Barbiturates / chemical synthesis
  • Barbiturates / history
  • Barbiturates / therapeutic use
  • Chemistry, Organic / history
  • Chemistry, Pharmaceutical / history*
  • Chloral Hydrate / chemical synthesis
  • Chloral Hydrate / history
  • Chloral Hydrate / therapeutic use
  • Chloroform / chemical synthesis
  • Chloroform / history
  • Chloroform / therapeutic use
  • Drug Discovery / history*
  • Drug Industry / history
  • History, 18th Century
  • History, 19th Century
  • History, 20th Century
  • History, Ancient
  • Humans
  • Pharmaceutical Preparations / chemical synthesis
  • Pharmaceutical Preparations / history
  • Pharmacology / history
  • Plant Preparations / chemistry
  • Plant Preparations / history
  • Plant Preparations / isolation & purification
  • Plant Preparations / therapeutic use
  • Toxicology / history


  • Alkaloids
  • Analgesics
  • Antipyretics
  • Barbiturates
  • Pharmaceutical Preparations
  • Plant Preparations
  • Chloral Hydrate
  • Chloroform
  • Aspirin